Table 5.
In vitro activities of liposomal AmB formulations prepared from DSHemsPC against L. major promastigotes and amastigotes
| ED50 for L. major (μg/ml, Lower and Upper 95% limit) |
||
|---|---|---|
| AmB formulations | Promastigotes | Amastigote |
| F1-DSHemsPC/DSPC/DSPG/AmB | 8(1.7–38.3) | 5.55(2.5–12.5) |
| F2-DSHemsPC/DSPC/DSPG/AmB | 6.8(1–46) | 5.046(2.3–11.2) |
| F3-DSHemsPC/DSPC/DSPG/AmB | 11.3(6.4–19.9) | 5.64(4.4–7.3) |
| F4-DSHemsPC/DSPC/DSPG/AmB | 6.51(1.3–31.9) | 4.03(2.1–7.9) |
| F5-DSHemsPC/DPPC/DPPG/AmB | 12.4(1.5–103.3) | 9.8(4.5–21.6) |
| F6-DSHemsPC/DPPC/DPPG/AmB | 19.6(3.1–127) | 9.6(5.4–17.1) |
| F7-DSHemsPC/DPPC/DPPG/AmB | 7.7(1.1–54) | 6.59(4.9–8.8) |
| F8-DSHemsPC/DPPC/DPPG/AmB | 7.9(2.9–21.1) | 6.47(4–10.5) |
| F9-DSHemsPC/DMPC/DMPG/AmB | 3.6(0.4–33.2) | 2.97(2.3–3.9) |
| F10-DSHemsPC/DMPC/DMPG/AmB | 4.8(2.2–10.4) | 4.28(3.2–5.8) |
| F11-DSHemsPC/DMPC/DMPG/AmB | 3.1(0.8–12.3) | 2.8(2.3–3.6) |
| F12-DSHemsPC/DMPC/DMPG/AmB | 4.9(0.6–40.3) | 2.14(1.7–2.7) |
| F13-DSHemsPC/HSPC/DSPG/AmB | 7.4(1–56.2) | 4.6(3.4–6.2) |
| F14-DSHemsPC/HSPC/DSPG/AmB | 8.5(1.8–40.1) | 4.85(3.2–7.5) |
| F15-DSHemsPC/HSPC/DSPG/AmB | 11.8(2.1–66.5) | 11.1(6.1–20.2) |
| F16-DSHemsPC/HSPC/DSPG/AmB | 8.9(2.1–37.5) | 6.3(4.3–9.3) |
| F17-DSHemsPC/HSPC/DSPG/AmB | 15.6(5.1–47.0) | 14.88(7.8–28.3) |
| F18-DSHemsPC/HSPC/DSPG/AmB | 12.8(2.7–60.8) | 9.5(7.4–12.3) |
| F19-DSHemsPC/HSPC/DSPG/AmB | 6.8(3.1–14.5) | 4.15(3.1–5.6) |
| F20-DSHemsPC/HSPC/DSPG/AmB | 6.5(2.65–16) | 4.1(2.8–6.1) |
|
| ||
| F21-DSHemsPC/DSPC/DSPG/AmB | 1.2 (0.8–2) | 0.185(0.13–0.3) |
| F22-DSHemsPC/DPPC/DPPG/AmB | 5.6 (4.9–7.7) | 0.732(0.5–1.2) |
| F23-DSHemsPC/DMPC/DMPG/AmB | 3.5 (2.1–6.8) | 0.76(0.5–1.1) |
| F24-DSHemsPC/DMPC/DMPG/AmB | 0.875 (0.7–2.1) | 0.24(0.058–1.08) |
| F25-DSHemsPC/HSPC/DSPG/AmB | 1.3 (0.7–2.1) | 0.21(0.1–0.34) |
| F26-DSHemsPC/HSPC/DSPG/AmB | 1.3(0.7–2.1) | 0.16(0.1–0.3) |
|
| ||
| F27-DSHemsPC/DSPC/DSPG/AmB | 1.3 (0.7–2.1) | 0.163(0.1–0.3) |
| F28-DSHemsPC/DPPC/DPPG/AmB | 1.8 (1.4–2.8) | 0.218(0.1–0.4) |
| F29-DSHemsPC/DMPC/DMPG/AmB | 1.4(0.7–4.9) | 0.14(0.1–0.2) |
| F30-DSHemsPC/DMPC/DMPG/AmB | 1.5 (0.7–2.8) | 0.168(0.1–0.3) |
| F31-DSHemsPC/HSPC/DSPG/AmB | 4.2(3.5–5.6) | 0.56(0.4–0.7) |
| F32-DSHemsPC/HSPC/DSPG/AmB | 2(1.4–3.5) | 0.208(0.2–0.3) |
| F33-DSHemsPC/DMPC/DMPG | Inactive | Inactive |
| AmBisome ™ | 1.4 (0.8–2.7) | 0.86(0.6–1.2) |
| Fungizone™ | 0.24 (0.1–0.9) | 0.108(0.16–0.7) |
Promastigotes assay: The ED50 of F1–F8, F13–F20, F22, F23, and F31 was significantly (P < 0.001) greater than AmBisome™ and Fungizone™. The ED50 of F21, F24–F30, and F32 was similar (P > 0.05) to AmBisome™. The ED50 of F24 and F27 was similar (P > 0.05) to Fungizone™.
Amastigote assay: The ED50 of F5–F8, and F15–F18 was significantly (P < 0.01) greater than AmBisome™ and Fungizone™. There were no significant (P > 0.05) differences in the activities of the F1–F4, F9–F14, F19, F20, F22 and F23 formulations against L. major amastigotes compare to AmBisome™. The ED50 of F5–F8, and F15–F18 was significantly (P < 0.001) greater than AmBisome™ and Fungizone™. The ED50 of F21, F24–F30, and F32 was similar (P > 0.05) to Fungizone™.